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Ipatasertib dihydrochloride

Catalog No. T15374 CAS 1396257-94-5

Synonyms: GDC-0068 dihydrochloride, RG-7440 dihydrochloride

Ipatasertib dihydrochloride (GDC-0068 dihydrochloride) is a highly selective and ATP-competitive inhibitor of pan-Akt (IC50s: 5, 18 and 8 nM for Akt1, Akt2 and Akt3, respectively).

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Ipatasertib dihydrochloride Chemical Structure

Ipatasertib dihydrochloride, CAS 1396257-94-5

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5 mg	In stock	$ 55.00
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1 mL * 10 mM (in DMSO)	In stock	$ 67.00

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Description	Ipatasertib dihydrochloride (GDC-0068 dihydrochloride) is a highly selective and ATP-competitive inhibitor of pan-Akt (IC50s: 5, 18 and 8 nM for Akt1, Akt2 and Akt3, respectively).
Targets&IC50	Akt3:8 nM, PKA:3100 nM, Akt2:18 nM, Akt1:5 nM
In vitro	Ipatasertib displays more than 600 and more than 100-fold selectivity for Akt1 in IC50 against the closely related kinases PKA and p70S6K, respectively. Ipatasertib inhibits only 3 other kinases by more than 70% at 1 μM concentration (PRKG1α, PRKG1β, and p70S6K) when tested at 1 μM in a panel of 230 protein kinases, which includes 36 human AGC family members. IC50s measured for these 3 kinases are 98, 69, and 860 nM, respectively. The relationship between pharmacokinetics (PK) and pharmacodynamics (PD) of Ipatasertib is investigated in 3 xenograft models that showed a dose-dependent response to drug treatment: MCF7-neo/HER2, TOV-21G.x1, and LNCaP. The mean cell viability IC50 of Ipatasertib in these 3 cell lines is 2.56, 0.44, and 0.11 μM, respectively. Ipatasertib shows a more than 100-fold selectivity for Akt1 over the next most potently inhibited non-Akt kinase, p70S6K, in the screening kinase panel with the exception of PKG1 (relative to which Ipatasertib is >10-fold more selective for Akt1) [2].
In vivo	Ipatasertib is typically efficacious in xenograft models in which Akt is activated because of genetic alterations including PTEN loss, PIK3CA mutations/amplification, or HER2 overexpression. The combination of Ipatasertib with RP-56976 or NSC 241240 is tolerated with less than 5% body weight loss when compared with treatment with each chemotherapeutic agent alone. The daily dosing of Ipatasertib in combination with RP-56976 induces tumor regression and stasis in the PC-3 and MCF7-neo/HER2 xenograft models, at doses where every single agent is ineffective or only causes modest tumor growth delay, when tested in vivo. Similarly, enhanced TGI is observed in the OVCAR3 ovarian cancer xenograft model when Ipatasertib is combined with NSC 241240 [2].

Synonyms	GDC-0068 dihydrochloride, RG-7440 dihydrochloride
Molecular Weight	530.92
Formula	C24H34Cl3N5O2
CAS No.	1396257-94-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 125 mg/mL (235.44 mM), Sonification is recommended.

H2O: 41 mg/mL (77.22 mM)

References and Literature

1. Blake JF, et al. Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors. J Med Chem. 2012 Sep 27;55(18):8110-27. 2. Lin J, et al. Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models. Clin Cancer Res. 2013 Apr 1;19(7):1760-72.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Inhibitor Library Tyrosine Kinase Inhibitor Library Anti-Cancer Active Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Antioxidant Compound Library Clinical Compound Library Glycolysis Compound Library Bioactive Compound Library

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Keywords

Ipatasertib dihydrochloride 1396257-94-5 Cytoskeletal Signaling PI3K/Akt/mTOR signaling Tyrosine Kinase/Adaptors Akt PKA RG 7440 Inhibitor PKB GDC 0068 Dihydrochloride Ipatasertib Dihydrochloride RG-7440 GDC 0068 RG7440 Dihydrochloride inhibit GDC-0068 Dihydrochloride RG-7440 Dihydrochloride GDC-0068 Ipatasertib RG7440 GDC-0068 dihydrochloride RG-7440 dihydrochloride Protein kinase B GDC0068 Dihydrochloride RG 7440 Dihydrochloride GDC0068 inhibitor

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